Structures, properties, and activities of EPIs optimized against MexAB-OprM. The top table shows the values of efflux inhibition predictors calculated for the indicated compounds. Values highlighted in green show desired changes, and those in yellow to orange show undesired changes. The bottom table shows the antibacterial (MIC) and EPI (MPC4 and SS50 µM/SS0 µM) activities of indicated compounds (CAR, carbenicillin; CTX, cefotaxime; LVX, levofloxacin; CIP, ciprofloxacin; NOV, novobiocin). Values highlighted in green show desired changes, and those in red show undesired changes. MICs were measured in efflux-deficient PΔ6-Pore cells and their complemented derivative carrying the plasmid-borne MexAB-OprM. MPC4 activities were analyzed in the complemented PΔ6-Pore(MexAB-OprM). CC50 (50% cytotoxic concentration) values with asterisks are from reference 50.